U.S. patent application number 13/793177 was filed with the patent office on 2014-06-12 for hoya carnosa extracts and methods of use.
This patent application is currently assigned to AVON PRODUCTS, INC.. The applicant listed for this patent is AVON PRODUCTS, INC.. Invention is credited to Ying Chen, Cheng S. Hwang, Jolanta Idkowiak-Baldys, John W. Lyga, Uma Santhanam, Qian Zheng.
Application Number | 20140161911 13/793177 |
Document ID | / |
Family ID | 50881202 |
Filed Date | 2014-06-12 |
United States Patent
Application |
20140161911 |
Kind Code |
A1 |
Zheng; Qian ; et
al. |
June 12, 2014 |
Hoya Carnosa Extracts and Methods of Use
Abstract
Methods of using extracts of Hoya carnosa to impart anti-aging
benefits to skin and/or improve skin conditions resulting from
aging or damaged skin.
Inventors: |
Zheng; Qian; (Morris Plains,
NJ) ; Lyga; John W.; (Basking Ridge, NJ) ;
Santhanam; Uma; (Tenafly, NJ) ; Chen; Ying;
(Towaco, NJ) ; Idkowiak-Baldys; Jolanta; (Franklin
Lakes, NJ) ; Hwang; Cheng S.; (New Milford,
NJ) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
AVON PRODUCTS, INC. |
Suffern |
NY |
US |
|
|
Assignee: |
AVON PRODUCTS, INC.
Suffern
NY
|
Family ID: |
50881202 |
Appl. No.: |
13/793177 |
Filed: |
March 11, 2013 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
PCT/US12/68865 |
Dec 11, 2012 |
|
|
|
13793177 |
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Current U.S.
Class: |
424/725 |
Current CPC
Class: |
A61K 8/9789 20170801;
A61Q 19/02 20130101; A61Q 19/08 20130101 |
Class at
Publication: |
424/725 |
International
Class: |
A61K 8/97 20060101
A61K008/97; A61Q 19/08 20060101 A61Q019/08 |
Claims
1. A method of improving the aesthetic appearance of an aging skin
in need thereof, comprising topically applying to the skin a
topical composition comprising: (a) a Hoya carnosa plant extract;
(b) a cosmetically, dermatologically, pharmaceutically, or
physiologically acceptable vehicle. in an amount effective to
improve the aesthetic appearance of skin.
2. The method according to claim 1, wherein aging is due to
chronological, hormonal, or environmental effects.
3. The method according to claim 1, wherein the improvement in
aesthetic appearance is improvement in skin tone, radiance, clarity
and/or tautness, skin firnmess, plumpness, suppleness, and/or
softness, skin texture and/or promotion of skin retexturization and
moisturization; appearance of skin contours, hollow cheeks, sunken
eyes, restoration of skin luster and/or brightness; replenishment
of essential nutrients and/or constituents in the skin decreased by
aging and/or menopause; increase in cell proliferation and/or
multiplication; increase in cell metabolism decreased by aging
and/or menopause; enhancement of skin thickness; reducing skin
sensitivity; an increase in skin elasticity and/or resiliency,
treatment, reduction and/or prevention of a sunken facial
appearance, or combinations thereof.
4. The method according to claim 1, wherein the skin is sensitive
skin.
5. The method according to claim 1, wherein the composition is
topically applied at least once daily for at least one week.
6. The method according to claim 1, wherein the extract is present
in an amount about 0.0001 wt % to about 90 wt % based on the total
weight of the composition.
7. The method according to claim 1, wherein the extract is present
in an amount of from about 0.01 wt % to about 10 wt % of the total
weight of the composition.
8. The method according to claim 1, wherein the Hoya carnosa plant
extract is derived from the whole of the Hoya carnosa plant.
9. The method according to claim 1, wherein the improvement of the
skin is due to an increase in collagen proliferation, increase in
epidermis thickness, increase in lipid accumulation, or any
combination thereof.
10. A method for improving the barrier function and viability of
the skin, comprising topically applying to the skin the composition
according to claim 1 in an amount effective to increase collagen
synthesis, increase epidermis thickness, or any combination
thereof.
11. The method according to claim 10, wherein the extract is
derived from the whole of the Hoya carnosa plant.
12. The method according to claim 10, wherein the plant extract is
present in an amount of about 0.0001 wt % to about 90 wt % based on
the total weight of the composition.
13. The method according to claim 10, wherein the plant extract is
present in an amount of about 0.01 wt % to about 10 wt % based on
the total weight of the composition.
14. A method of treating wrinkles, fine lines, or a sagging skin,
comprising topically applying to the skin the composition according
to claim 1 in an amount effective to treat the skin in need
thereof.
15. A method of treating skin comprising topically applying to an
area of the skin in need thereof an effective amount of a Hoya
carnosa extract that modulates a skin biomarker, wherein the
ability of the Hoya carnosa extract to modulate a skin biomarker
has been determined by an assay which measures the amount of change
in a skin biomarker selected from the group comprising epidermal
thickening; total collagen; and pro-collagen in skin cells and/or
skin cell pre-differentiation precursors that have been contacted
with the Hoya carnosa extract.
16. A method for treating a skin condition characterized by
insufficient subcutaneous lipids, comprising topically applying to
skin in need thereof an effective amount of at least one Hoya
carnosa extract in a cosmetically acceptable vehicle for a time
sufficient to improve the aesthetic appearance of said skin.
Description
RELATED APPLICATION
[0001] This application claims priority to the following patent
application as a continuation-in-part: PCT Application Serial No.
PCT/US2012/68865, entitled "Hoya carnosa Extracts and Methods of
Use", filed on Dec. 11, 2012 and naming Qian Zheng as first
inventor, the entirety of which is incorporated by reference herein
in its entirety for all purposes.
[0002] The following patent applications are herein incorporated by
reference in their entirety for all purposes: PCT Application
Serial No. PCT/US12/68856, entitled "Callistephus chinensis
extracts and methods of use", filed Dec. 11, 2012 and naming Qian
Zheng as first inventor; PCT Application Serial No. PCT/US12/68858,
entitled "Serissa japonica extracts and methods of use", filed on
Dec. 11, 2012 and naming Qian Zheng as first inventor; U.S.
application Ser. No. 13/710,617, entitled "Medemia nobilis extracts
and methods of use for improving the condition and appearance of
skin and other keratinous materials", filed on Dec. 11, 2012 and
naming Permanan Raaj Khusial as first inventor.
FIELD OF INVENTION
[0003] The present invention relates generally to cosmetic
compositions incorporating Hoya carnosa extracts and their use to
reduce fine lines and wrinkles, improve sagging, enhance lifting,
and improve skin tone and to improve the overall appearance of skin
by increasing epidermis thickness and stimulating the production of
collagen, and/or by inducing lipogenesis.
BACKGROUND OF THE INVENTION
[0004] Consumers are increasingly interested in cosmetics that
treat, mitigate, or delay the signs of aging or aged skin. The
signs of aging or aged skin manifest themselves in lines and
wrinkles, sagging, dullness, discoloration, uneven tone, and/or
rough texture. Further, aged skin lacks strength and elasticity and
is therefore fragile. The cosmetics industry is actively pursuing
products that may be used to reduce signs of aging or aged skin
(anti-aging compounds) and thereby provide anti-wrinkle, and skin
rejuvenating benefits.
[0005] Human skin is broadly divided into two layers: the surface
epidermis which provides an anatomical barrier to foreign elements
and maintains the body's internal environment, and the underlying
dermis which provides nutritional and structural support to the
epidermis. The epidermis mainly consists of keratinocytes and is
comprised of several sub-layers (from the innermost outwards):
Stratum germinativum/Stratum basale, Stratum spinosum, Stratum
granulosum, and Stratum corneum. The keratinocytes, generated by
the mitosis of keratinocyte stem cells, originate in the stratum
basale and then push up through the strata. As these cells move to
the surface of the skin they undergo gradual differentiation,
becoming anucleated, flattened, and highly keratinized. During this
process the keratinocytes become highly organized. They form
desmosomes, cellular junctions, between each other and, through the
excretion of keratin proteins and lipids, form an extracellular
matrix which strengthens the skin. Eventually the keratinocytes die
off and form the stratum corneum. In healthy skin, keratinocytes
are shed and replaced continuously every 30 days.
[0006] The dermis is the underlying layer of the skin located
between the epidermis and subcutaneous tissue. Since the epidermis
lacks blood vessels, the cells of the epidermis rely upon the blood
vessels in the dermis for their nutrients and oxygen. The
dermal-epidermal junction (DEJ) is a specialized structure that
maintains close contact between the lamina densa, a layer of
extracellular matrix upon which the epithelium sits, and the
underlying connective tissue of the dermis. The DEJ is comprised
mainly of collagen and elastin and structured as interlocking
finger-like projections from the epidermis and dermal layers called
Rete ridges. The Rete ridges increase the surface area of the
epidermis exposed to the dermis at the DEJ, so that the transfer of
necessary nutrients/oxygen is more efficient, and the two layers of
the skin form a strong bond that resists mechanical stress (shear).
Additionally, the dermis is the thickest of the skin layers and
comprises the extracellular matrix of the skin, which is maintained
by fibroblast cells. Fibroblasts maintain the structural integrity
of connective tissues by continuously secreting precursors of the
extracellular matrix. The main structural component of the dermis
is a protein called collagen. Bundles of collagen molecules pack
together throughout the dermis, accounting for three-fourths of the
dry weight of skin. Collagen has great tensile strength; along with
soft keratin, it is responsible for skin strength and elasticity.
For a more detailed background on collagen, see Lodish, et al.
Molecular Cell Biology, W.H. FREEMAN, New York, N.Y. 4th edition,
2000, the disclosures of which is incorporated herein by reference
in their entirety.
[0007] Histological studies of the skin show that as aging occurs,
the skin undergoes structural, functional, and metabolic changes
that parallel the aging and degenerative changes in other body
organs. While chronological and/or hormonal aging play a
significant role in skin aging, environmental stresses such as sun
exposure may initiate and/or accelerate the aging of the skin due
to, in part, oxidative damage from overexposure to ultraviolet (UV)
sunlight. In aged and/or aging skin the cells may take longer to
replenish, be less numerous, and/or breakdown more quickly. In
particular, as aging occurs, the production of collagen is reduced
while the degradation is accelerated due to an overproduction of
collagenase, i.e. a protease that breaks down collagen. The
resulting collagen deficiency may lead to reduction in skin
strength and elasticity. Further, given that collagen is a major
component of the DEJ, the DEJ flattens out with aging, such that
the skin is more fragile and more likely to shear. As the DEJ
flattens the amount of nutrients/oxygen transferred to the
epidermis through the DEJ is reduced because the surface area in
contact with the epidermis shrinks. The reduction of HA within the
epidermis extracellular matrix reduces the epidermis's ability to
transfer the available nutrients/oxygen to its cells. This
inefficient nutrient/oxygen transport impacts the keratinocytes of
the epidermis. The keratinocytes renewal rate is reduced and as a
consequence the stratum corneum loses its capacity to retain
moisture and the skin dehydrates. At the surface of the skin, aged
or aging skin may exhibit lines and wrinkles, sagging, dullness,
discoloration, uneven tone, rough texture, and the like.
Additionally, aged or aging skin exhibits less strength and
flexibility and is more fragile. These signs of aging may be
exacerbated by common medications such as those prescribed for the
treatment of Parkinson's disease, i.e. Levodopa, or menopause, i.e.
hormone therapies.
[0008] The skin, epidermis and dermis, are supported by a layer of
subcutaneous fat that insulates and cushions the body from external
forces. The subcutaneous fat is comprised of adipocytes (fat
cells), arranged in chambers or lobules separated by fibrous septa
Subcutaneous adipose tissue is crucial for maintaining facial
volume and fullness. Loss of subcutaneous fat that is associated
with pathological lipoatrophy or aging leads to facial sagging,
sunken appearance and wrinkles and folds on the face. Currently
dermatological procedures such as lipofilling and lipografting are
used to address loss of facial volume and correct facial contour.
The subcutaneous fat of the face is partitioned into discrete
anatomic compartments. Facial aging is, in part, characterized by
how these compartments change with age. It has been shown that with
aging (as well as with exposure to UV and oxidative stress) the
thin layer of fat under skin is damaged, leading to facial sagging
and aged look. On the cellular level it was shown that the ability
of preadipocytes to differentiate into mature adipocytes declines
with age.
[0009] Hoya carnosa, the wax plant, is a species in the dogbane
family (Apocynaceae). It is native to Eastern Asia and Australia.
Hoya carnosa has star-shaped light pink flowers covered in tiny
hairs that are borne in clusters. They are heavily scented.
[0010] There remains a need for cosmetic compositions which address
the signs of aging, in particular the appearance of wrinkles,
lines, and sagging, sagging, loss of firmness/cushion. It is
therefore an object of the present invention to provide new
compositions and methods for treating, ameliorating, and/or
preventing signs of aged or aging skin and/or stimulating lipid
production ("lipogenesis") in the skin, suitable for the treatment
and prevention of the loss of subcutaneous fat, and in particular,
facial fat loss, sagging skin, wrinkles, dry skin, and the like. It
is a further object of the invention to improve the overall
appearance of aging or aged skin.
[0011] The foregoing discussion is presented solely to provide a
better understanding of the nature of the problems confronting the
art and should not be construed in any way as an admission as to
prior art nor should the citation of any reference herein be
construed as an admission that such reference constitutes "prior
art" to the instant application.
SUMMARY OF THE INVENTION
[0012] In accordance with the foregoing objectives and others, it
has been found that extracts of Hoya carnosa are surprisingly
potent agonists of collagen production and epidermis thickening and
thus are beneficial agents against unwanted features associated
with aging or aged skin.
[0013] It has further surprisingly been found that compositions
comprising and extract of Hoya carnosa may stimulate lipid
production ("lipogenesis") in the skin. Such compositions will be
particularly suitable for the treatment and prevention of the loss
of subcutaneous fat, and in particular, facial fat loss, sagging
skin, wrinkles, dry skin, and the like.
[0014] One embodiment of the current invention relates to a topical
composition including a Hoya carnosa plant extract; and a
cosmetically, dermatologically, pharmaceutically, or
physiologically acceptable vehicle. In a further embodiment, the
plant extract may be from the whole of the Hoya carnosa plant. In
certain embodiments, the composition may be an aerosol spray,
cream, emulsion, solid, liquid, dispersion, foam, gel, lotion,
mousse, ointment, powder, patch, pomade, solution, pump spray,
stick or towelette.
[0015] In another embodiment, the plant extract may be present in
the composition in an amount sufficient to increase collagen
proliferation, increase epidermis thickness, or any combination
thereof. In one embodiment, the plant extract may be present in an
amount from about 0.0001 wt % to about 90 wt %, based on the total
weight of the composition, and in a further embodiment, the plant
extract may be present in an amount from about 0.01 wt % to about
10 wt %, based on the total weight of the composition. In certain
embodiments, the plant extract may be in an amount sufficient to
alleviate the aesthetic appearance of wrinkles, pigment spots, skin
sagging, loss of skin elasticity, mottled skin appearance or any
combination thereof.
[0016] A further embodiment of the current invention relates to a
method of improving the aesthetic appearance of an aging skin in
need thereof, by topically applying to the skin the above-noted
composition in an amount effective to improve the aesthetic
appearance of skin. In one embodiment, the skin is sensitive skin.
In a further embodiment of the invention, the composition is
topically applied to the skin at least once daily for at least one
week.
[0017] In another embodiment, compositions incorporating Hoya
carnosa extracts are used to ameliorate, inhibit, delay, reduce,
and/or improve the signs of subcutaneous fat loss, and accordingly
find use as potent lipogenic products, and in particular aesthetic
facial appearance improvement products.
[0018] In certain embodiments the aging may be due to
chronological, hormonal, or environmental effects. In further
embodiments, the improvement in aesthetic appearance is selected
from the group of: (a) treatment, reduction, and/or prevention of
fine lines or wrinkles; (b) reduction of skin pore size; (c)
improvement in skin thickness, plumpness, and/or tautness; (d)
improvement in skin suppleness and/or softness; (e) improvement in
skin tone, radiance, and/or clarity; (f) improvement in procollagen
and/or collagen production; (g) improvement in maintenance and
remodeling of elastin; (h) improvement in skin texture and/or
promotion of re-texturization; (i) improvement in skin barrier
repair and/or function; (j) improvement in appearance of skin
contours; (k) restoration of skin luster and/or brightness; (l)
replenishment of essential nutrients and/or constituents in the
skin; (m) improvement of skin appearance decreased by aging and/or
menopause; (n) improvement in skin moisturization and/or hydration;
(o) increase in and/or preventing loss of skin elasticity and/or
resiliency; (p) treatment, reduction, and/or prevention of skin
sagging; (q) treatment, reduction, and/or prevention of
discoloration of skin; (r) treatment, reduction, and/or prevention
of a sunken facial appearance; and (s) any combination thereof. In
other embodiments of the current invention the improvement of the
skin may be due to an increase in collagen synthesis, an increase
epidermis thickness, an increase in lipid accumulation; or any
combination thereof.
[0019] In yet another embodiment of the invention, the extract may
be present in an amount from about 0.0001 wt % to about 90 wt %
based on the total weight of the composition, and in a further
embodiment may be present in an amount of from about 0.01 wt % to
about 10 wt % of the total weight of the composition. In certain
embodiments, the Hoya carnosa plant extract may be derived from the
whole of the Hoya carnosa plant.
[0020] Another embodiment of the current invention is directed to a
method of improving the barrier function and viability of the skin
by topically applying to the skin the above-noted composition in an
amount effective to increase collagen synthesis, increase epidermis
thickness, or any combination thereof. In a certain embodiment of
this method the extract is derived from whole of the Hoya carnosa
plant. In further embodiments of the method, the plant extract is
present in an amount of about 0.0001 wt % to about 90 wt % based on
the total weight of the composition, and in still further
embodiments, the plant extract is present in an amount of about
0.01 wt % to about 10 wt % based on the total weight of the
composition.
[0021] A further embodiment of the current method is directed to
treating wrinkles, fine lines, or a sagging skin, by topically
applying to the skin the above-noted composition in an amount
effective to treat the skin in need thereof.
[0022] A further embodiment of the current invention is directed to
a method of treating skin comprising topically applying to an area
of the skin in need thereof an effective amount of a Hoya carnosa
extract that modulates a skin biomarker, wherein the ability of the
Hoya carnosa extract to modulate a skin biomarker has been
determined by an assay which measures the amount of change in a
skin biomarker selected from the group comprising epidermal
thickening; total collagen; and pro-collagen in skin cells and/or
skin cell pre-differentiation precursors that have been contacted
with the Hoya carnosa extract.
[0023] In another embodiment, a method for treating a skin
condition characterized by insufficient subcutaneous lipids is
provided, comprising topically applying to skin in need thereof an
effective amount of at least one Hoya carnosa extract in a
cosmetically acceptable vehicle for a time sufficient to improve
the aesthetic appearance of said skin.
[0024] These and other aspects of the present invention will be
better understood by reference to the following detailed
description and accompanying figures.
BRIEF DESCRIPTION OF THE DRAWINGS
[0025] FIG. 1 is a HPLC profile of an extract of Hoya carnosa.
DETAILED DESCRIPTION
[0026] Detailed embodiments of the present invention are disclosed
herein; however, it is to be understood that the disclosed
embodiments are merely illustrative of the invention that may be
embodied in various forms. In addition, each of the examples given
in connection with the various embodiments of the invention are
intended to be illustrative, and not restrictive. Further, the
figures are not necessarily to scale, and some features may be
exaggerated to show details of one embodiment components. In
addition, any measurements, specifications and the like shown in
the figures are intended to be illustrative, and not restrictive.
Therefore, specific structural and functional details disclosed
herein are not to be interpreted as limiting, but merely as a
representative basis for teaching one skilled in the art to
variously employ the present invention.
[0027] The successful restoration of youthful skin must address a
variety of key issues including: vitality of fibroblasts and
keratinocytes, cell-cell adhesion in the epidermis and dermis, cell
nourishment to the epidermis, cell-cell anchoring and adhesion
between keratinocytes, communication between the dermis and
epidermis, collagenase overproduction, collagen replacement, and
mechanical properties of the skin. The present invention addresses
these key issues through the use of cosmetic compositions
incorporating extracts of Hoya carnosa. In particular, the
compositions of the current invention are used to reduce fine
lines, wrinkles, and sagging, and improve skin tone and to improve
the overall appearance of skin. The extracts of Hoya carnosa
stimulate the production of collagen and/or increase epidermis
thickness.
[0028] The present invention provides compositions for topical
application which comprise an effective amount of an extract of
Hoya carnosa to treat, reverse, ameliorate and/or prevent signs of
skin damage or skin aging. Such benefits include without
limitation, the following:
[0029] (a) treatment, reduction, and/or prevention of fine lines or
wrinkles,
[0030] (b) reduction of skin pore size,
[0031] (c) improvement in skin thickness, plumpness, and/or
tautness;
[0032] (d) improvement in skin suppleness and/or softness;
[0033] (e) improvement in skin tone, radiance, and/or clarity;
[0034] (f) improvement in procollagen and/or collagen
production;
[0035] (g) improvement in maintenance and remodeling of
elastin;
[0036] (h) improvement in skin texture and/or promotion of
re-texturization;
[0037] (i) improvement in skin barrier repair and/or function;
[0038] (j) improvement in appearance of skin contours;
[0039] (k) restoration of skin luster and/or brightness;
[0040] (l) replenishment of essential nutrients and/or constituents
in the skin;
[0041] (m) improvement of skin appearance decreased by aging and/or
menopause;
[0042] (n) improvement in skin moisturization and/or hydration;
[0043] (o) increase in and/or preventing loss of skin elasticity
and/or resiliency;
[0044] (p) treatment, reduction, and/or prevention of skin
sagging;
[0045] (q) treatment, reduction, and/or prevention of discoloration
of skin; and/or
[0046] (r) treatment, reduction, and/or prevention of a sunken
facial appearance.
[0047] In practice, the compositions of the invention are applied
to skin in need of treatment. That is, skin which suffers from a
deficiency or loss in any of the foregoing attributes or which
would otherwise benefit from improvement in any of the foregoing
skin attributes.
[0048] In one embodiment, the composition is intended for use as a
non-therapeutic treatment. In another embodiment, the composition
is an article intended to be rubbed, poured, sprinkled, or sprayed
on, introduced into, or otherwise applied to the human body for
cleansing, beautifying, promoting attractiveness, or altering the
appearance, in accordance with the US FD&C Act, sec.
201(i).
[0049] All terms used herein are intended to have their ordinary
meaning unless otherwise provided.
[0050] The term "active amount" refers to the amount of Hoya
carnosa extract absent diluent, solvent, carrier, filler or any
other ingredient. An "amount effective" or an "effective amount" to
provide a particular anti-aging benefit to the skin refers to the
"active amount" of extract required to provide a clinically
measurable improvement in the particular manifestation of aging,
i.e., an unwanted feature associated with aging, when applied or
administered for a time sufficient to provide a clinically
measurable improvement in the particular manifestation of
aging.
[0051] As used herein, the term "a person in need thereof" refers
to an individual with a normal but noticeable and undesired skin
condition, unwanted feature, due to aging, e.g. lines and wrinkles,
sagging, dullness, discoloration, uneven tone, rough texture, etc.,
or an individual that elects to decrease the effects of aging in
the absence of a noticeable and undesired skin condition, i.e. as a
preventative or prophylactic.
[0052] As used herein, the term "consisting essentially of" is
intended to limit the invention to the specified materials or steps
and those that do not materially affect the basic and novel
characteristics of the claimed invention, as understood from a
reading of this specification.
[0053] By "cosmetically acceptable" it is meant that a particular
component is generally regarded as safe and nontoxic at the levels
employed.
[0054] As used herein, the term "discoloration" includes discrete
pigmentation and mottled pigmentation. Discrete pigmentation are
distinct uniform areas of darker pigment and may appear as brown
spots or freckles on the skin and may include solar lentigo,
darkened spots on the skin caused by aging and the sun also known
as "liver spots," "senile freckles," or "age spots," or ephelis,
freckles. Mottled pigmentation are dark blotches that are larger
and more irregular in size and shape than discrete pigmentation and
may include conditions such as chloasma, melasma, skin
discolorations caused by hormones, i.e. as the result of pregnancy,
birth control pills, or estrogen replacement therapy. The
discoloration may be the result of external factors including, but
not limited to, UV-R, tanning and photoaging, drugs, and/or
chemicals, or internal factors including, but not limited to,
genetics, hormonal influences, and/or inflammation.
[0055] Elasticity of the skin refers to the springiness and
resilience of skin's ability to regain its original shape and size
after deformation. Elasticity of the skin may be evaluated by a
pinch test that can either cause deformation by stretching or
squeezing the skin.
[0056] As used herein, the term "essential oil" refers to the
volatile ethereal fraction obtained from a plant or plant part by a
physical separation process such as distillation or chromatographic
separation. The essential oils are typically terpenoids often
comprising monoterpenes and have the odor and flavor of the plant
from which they were extracted.
[0057] "Prevention" as used herein, as well as related terms such
as "prevent" or "preventing," refer to affording skin not yet
affected by the condition a benefit that serves to avoid, delay,
forestall, minimize, or reduce the recurrence/onset of one or more
unwanted features associated with the skin condition to be
prevented. Such preventative benefits include, for example,
delaying development and/or recurrence of the condition, or
reducing the duration, severity, or intensity of one or more
unwanted features associated with the condition if it eventually
develops. Use of the term "prevention" is not meant to imply that
all subjects in a subject population administered the cosmetic
composition will never be affected by or develop the cosmetic or
dermatologic conditions, damage, effect, or symptom, but rather
that the subject population will exhibit a reduction in the
cosmetic or dermatologic damages, effects, or symptoms. For
example, many flu vaccines are not 100% effective at preventing flu
in those administered the vaccine. Preventing aging refers to
affording not yet affected skin a benefit that serves to avoid,
delay, forestall, or minimize one or more unwanted features
associated with aging, such as reducing the extent of lines and
wrinkles, sagging, dullness, discoloration, uneven tone, rough
texture, and/or fragileness that eventually develops at the treated
area.
[0058] The term "skin" as used herein includes the skin on or in
the face, mouth, neck, chest, back, arms, hands, legs, and scalp.
"Thin skin" is intended to include skin that is thinned due to
chronological aging, menopause, or photo-damage.
[0059] "Treatment" as used herein, as well as related terms such as
"treat" or "treating," refers to eradicating, reducing,
ameliorating, or reversing one or more of the unwanted features
associated with the skin condition being treated, such that the
consumer perceives an improvement in the appearance of the skin or
other treatment benefit with respect to the condition. Treating
skin aging or damage refers to eradicating, reducing, ameliorating,
or reversing one or more of the unwanted features associated with
aging. Unwanted features associated with aging skin, e.g., lines
and wrinkles, sagging, dullness, uneven tone, discoloration, and/or
rough texture. Treatment benefits include, e.g., reducing the
appearance of lines, wrinkles, and/or sagging, restoring luster to
the skin, evening the tone of skin, softening the skin texture,
and/or reducing pigmentation. The present compositions and methods
are suitable for use in treating dermatological conditions of the
skin in numerous areas of the body, including, without limitation
the face, forehead, lips neck, arms hands, legs, knees, feet chest,
back, groin, buttocks, and the like. In one embodiment, the
compositions are applied to the face.
[0060] The term "wrinkle" or "wrinkling" refers to both fine
wrinkling and coarse wrinkling. Fine wrinkling or fine lines refers
to superficial lines and wrinkles on the skin surface. Coarse
wrinkling refers to deep furrows, particularly deep lines/wrinkles
on the face and around the eyes, including expression lines such as
frown lines and wrinkles, forehead lines and wrinkles, crow's feet
lines and wrinkles, nasolabial fold and marionette lines and
wrinkles. Forehead lines and wrinkles refer to superficial lines
and/or deep furrows on skin of the forehead. Crow's feet lines and
wrinkles refer to superficial lines and/or deep furrows on skin
around the eye area. Marionette lines and wrinkles refer to
superficial lines and/or deep furrows on skin around the mouth.
Wrinkles can be assessed for number, length, and depth of the
lines.
[0061] All percentages are by weight based on the total weight of
the composition, unless otherwise indicated.
[0062] Cosmetic Compositions
[0063] The cosmetic compositions used in the method of the current
invention comprise a botanical component derived from the Hoya
carnosa plant. Hoya carnosa plant may be in any form including, but
not limited to, the whole plant, a dried plant, a ground plant or
parts thereof, including but not limited to, seeds, needles,
leaves, roots, bark, cones, stems, rhizomes, callus cells,
protoplasts, organs and organ systems, and meristems, an extract, a
dried extract, a synthetic extract, or components and/or
constituents found in, or isolated from, the plant, and/or portions
of the plant, or extracts derived either directly or synthetically
from the plant, or any combinations thereof. For the cosmetic
compositions used in this invention the botanical component is in
one embodiment derived directly from the Hoya carnosa plants. The
botanical component may be in a pure form, a semi-pure form, or
unpurified form. The Hoya carnosa botanical component may be in the
form of a liquid, a semi-solid, or a solid consistency. In one
embodiment, the botanical component may be an essential oil.
[0064] In one embodiment, the raw materials may be collected from
the whole of the Hoya carnosa plants (i.e. stems, leaves, roots,
flowers, etc.), and in certain embodiments the raw materials are
primarily or solely obtained from the leaves and stems of Hoya
carnosa. In certain embodiments, the raw materials collected from
the Hoya carnosa plants are ground to small particle sizes. In
addition, the raw materials may be dried to reduce water content.
The raw materials may be air-dried, oven-dried, rotary evaporated
under vacuum, lyophilized, or dried by any other suitable method
known in the art.
[0065] The extract of Hoya carnosa may be obtained by distilling
the raw materials with a stripping agent. The stripping agent may
be a liquid that is miscible, immiscible, or partially miscible
with the desired extract from Hoya carnosa. Suitable stripping
agents include, but are not limited to the following: water;
alcohols (such as methanol, ethanol, propanol, butanol and the
like); glycols; ethers (such as diethyl ether, dipropyl ether, and
the like); esters (such as butyl acetate, ethyl acetate, and the
like); ketones (such as acetone, ethyl methyl ketone, and the
like); dimethyl sulfoxide; acetonitrile; other organic solvents;
and combinations thereof. In one embodiment, the stripping agent is
immiscible with the desired extract from Hoya carnosa. The Hoya
carnosa extract may be collected by phase separation from the
stripping agent. It is believed that the stripping agent increases
the overall vapor pressure of a distillation system for obtaining
an extract of Hoya carnosa and thereby reduces the boiling point of
the desired product, the Hoya carnosa extract.
[0066] In other embodiments, Hoya carnosa botanical component may
be in the form of an extract obtained by solvent extraction, in one
embodiment obtained by an organic solvent extraction. Briefly, the
organic solvent extraction method involves washing and extracting
the raw materials, which may be whole or ground into small particle
sizes, using an organic solvent. Non-limiting examples of organic
solvents include methanol, ethanol, isopropanol, dichloromethane,
chloroform, hexane, xylene, and petroleum ether. An extracting
machine may be used for organic solvent extraction as is well known
in the field. The raw materials are pushed slowly into the
extracting machine by a thruster. Organic solvent (e.g., ethanol)
may be added into the machine through a solvent inlet at the top of
a waste discharge outlet. Due to the difference in gravity and
equilibrium, the solvent flows toward the raw material inlet, soaks
the materials and flows out from the opposite side of the solvent
inlet. Since the plant materials and the solvent move in opposite
directions against each other, the plant materials are constantly
immersed in a solution that contains a low-concentration of
extract. As a result of equilibrium, high yield of plant
constituent(s) may be achieved by continuously extracting the plant
material against the low-concentration solution.
[0067] An extraction time suitable to extract the Hoya carnosa
plant constituents is used, typically between about 1-10 hours, in
one embodiment between about 2-8 hours, and in one embodiment
between about 3-6 hours. The temperature of extraction is between
about 30.degree. C.-100.degree. C., in one embodiment between about
40.degree. C.-70.degree. C., and in one embodiment between about
50.degree. C.-60.degree. C. The collected extract is then
fine-filtered to remove debris, and may be used directly, or is
concentrated, for example by distilling the solvent or by other
conventional processing. The solution of extract actives may be
rotary evaporated under vacuum or lyophilized. A typical extract's
actives content is above about 25%, in one embodiment above 50%,
and the extract may also be provided as an essential oil or a
concentrate having a semi-solid or solid consistency.
[0068] Similarly, aqueous-organic solvent extraction involves
initially collecting raw materials from the Hoya carnosa plants,
which may be whole or ground into small particle sizes. The ground
plant material is soaked in aqueous solution that is acidic or
alkaline, depending on the solubility and stability of the desired
extract under acidic or alkaline (basic) conditions. For extraction
under acidic conditions, an acid such as hydrochloric acid or
sulfuric acid is added to water, e.g., at a concentration of about
3% (w/v). For extraction under alkaline conditions, an alkali such
as sodium hydroxide or sodium carbonate is added to water. The
extraction time and temperature of extraction are typically similar
to that used in the organic solvent extraction method described
above.
[0069] The extract is then collected and fine-filtered to remove
debris. Alkaline agents (e.g., ammonia) or acidifying agents (e.g.,
sulfuric acid) may be added to the extract to neutralize the
solution by adjusting the pH, depending on the acidity or
alkalinity of the collected extract. The aqueous extract may be
used directly, in concentrated or dried form. Alternatively,
organic solvent may then be added to the neutralized solution to
transfer the extract from an aqueous phase to an organic phase.
Examples of such organic solvents include, but are not limited to,
ethanol, isopropanol, butanol, pentanol, hexanol, and xylene. The
extract comprising the transferred extract actives dissolved in
organic solvent may be used directly as an essential oil or a
concentrate, or dried by a number of different means, such as, for
example, air-drying, oven-drying, rotary evaporating under vacuum
or lyophilizing to a semi-solid or solid consistency.
[0070] It should also be noted that different plants containing
different constituents can be mixed and extracted together with
Hoya carnosa. This process of mixed extraction can in one
embodiment be used for extracting those plants containing
constituents with similar solubility as Hoya carnosa in the solvent
used for extraction, such as ethanol. The mixture of extracts can
be concentrated and stored in an appropriate solvent.
[0071] In another embodiment, the Hoya carnosa extract as used
herein, also includes "synthetic" extracts, i.e., various
combinations of known Hoya carnosa plant components and/or
constituents that are combined to substantially mimic the
composition and/or activity of a Hoya carnosa plant extract of
natural origin. In one embodiment, the synthetic extracts have
substantially the same number of active components as a natural
Hoya carnosa plant material. The correspondence of the numerical
incidence of actives between the synthetic extracts and the natural
Hoya carnosa plant material may also be described in terms of
"percent commonality." The synthetic extract has about 50 percent
or more commonality to the chemical composition of a plant or
natural extract. In other words, the synthetic extract has about 50
percent or more of the active ingredients found in the plant or a
natural extract. In one embodiment, the chemical composition of the
synthetic extract has about 70 percent or more commonality to the
chemical composition of a plant or a natural extract. Optimally, a
synthetic extract has about 90 percent or more commonality to the
chemical composition of a plant or a natural extract.
[0072] The compositions according to the invention can be
formulated in a variety of forms for topical application and will
comprise from about 0.0001% to about 90% by weight of an extract of
Hoya carnosa, and in one embodiment will comprise from about
0.0005% to about 25% by weight, and in one embodiment from about
0.001% to about 10% by weight. In one embodiment range, the
composition may comprise a Hoya carnosa extract within a range from
about 0.005%, 0.01%, 0.05%, 0.1%, 0.25%, 0.5%, 0.75% or 1% up to
5%, 7.5% or 10% by weight of the total composition. The
compositions will comprise an effective amount of an extract of
Hoya carnosa, by which is meant an amount sufficient to reduce
and/or inhibit the appearance of signs of aging or damage in a
given area of skin when topically applied thereto. The above
amounts refer to an "active amount" of a Hoya carnosa extract.
[0073] In accordance with the invention, compositions comprising
components from the Hoya carnosa plant include, but are not limited
to, topically applied formulations, anti-oxidants,
anti-inflammatories, sunscreens, cosmetics (including makeup),
personal care products (e.g., antiperspirants or deodorants for
controlling body odor), topicals, skin penetration enhancers, and
the like. Also in accordance with this invention, the Hoya carnosa
plant components and additional ingredients comprising such
compositions may be formulated in a variety of product forms. The
compositions may be prepared in targeted delivery systems, e.g.
creams, lotions, gels, toners, serums, transdermal patches, and the
like, particularly for topical administration. Targeted delivery
and/or penetration enhancement may also be achieved by
iontophoresis.
[0074] The present invention further provides the compositions
comprising the Hoya carnosa plant components for the current method
be in one embodiment topically administered for targeted delivery.
The method of the current invention is suitable for all skin types,
such as sensitive, normal, oily, or combination. In particular
embodiments, the compositions may be in one embodiment applied to
sensitive skin or hair types. The compositions are applied to the
skin or hair for a period of time sufficient to improve the
aesthetic appearance of conditions related to skin, including
unwanted features associated aging, e.g. lines and wrinkles,
sagging, dullness, uneven tone, discoloration, and/or rough
texture. The compositions may be applied topically once, twice, or
more daily, in one embodiment once a day. The daily application may
be applied for a period of one week, two weeks, four weeks, or
more.
[0075] The compositions may be formulated into liposomes which can
comprise other additives or substances, and/or which can be
modified to more specifically reach or remain at a site following
administration. The compositions of the present invention yield
improvements to the aesthetic appearance by treating at least one
of the unwanted features related to skin aging or damage.
[0076] Another embodiment of the method of the current invention
encompasses compositions comprising a cosmetically or
dermatologically acceptable formulation which is suitable for
contact with living animal tissue, including human tissue, with
virtually no adverse physiological effect to the user. Compositions
embraced by this invention can be provided in any cosmetically
and/or dermatologically suitable form, in one embodiment as a
lotion or cream, but also in an anhydrous or aqueous base, as well
as in a sprayable liquid form. Other suitable cosmetic product
forms for the compositions used in this invention include, for
example, an emulsion, a cream, a balm, a gloss, a lotion, a mask, a
serum, a toner, an ointment, a mousse, a patch, a pomade, a
solution, a spray, a wax-based stick, or a towelette. In addition,
the compositions can include one or more compatible cosmetically
acceptable adjuvants commonly used and known by the skilled
practitioner, such as colorants, fragrances, emollients,
humectants, preservatives, vitamins, chelators, thickeners, perilla
oil or perilla seed oil (WO 01/66067 to a "Method of Treating a
Skin Condition," incorporated herewith in its entirety for all
purposes) and the like, as well as other botanicals such as aloe,
chamomile, and the like, and as further described below.
[0077] Also, embraced by the invention are transdermal modes of
delivery, such as patches and the like, with or without a suitable
penetration enhancer. The methods and compositions embodied by the
invention provide a means by which the Hoya carnosa components can
be effectively administered in a transdermal system. Accordingly, a
transdermal means of delivering a composition or formulation (often
with a penetration enhancing composition) to the skin is that of
the transdermal patch or a similar device as known and described in
the art. Transdermal patches are designed to deliver an effective
amount of compound across a user's skin. Transdermal patches
typically involve a liquid, gel, solid matrix, or
pressure-sensitive adhesive carrier into which the Hoya carnosa
extract may be incorporated. Patch formulations and preparations
are well known in the art. See for example "Dermatological and
Transdermal Formulations" (Drugs and the Pharmaceutical Sciences,
Vol 119) by Kenneth A Walters (Editor), Marcel Dekker and
"Transdermal Drug Delivery" (Drugs & the Pharmaceutical
Sciences) by Richard H. Guy (Editor), Jonathan Hadgraft (Editor)
2nd Rev & ex edition Marcel Dekker and "Mechanisms of
Transdermal Drug Delivery" (Drugs & the Pharmaceutical
Sciences, Vol 83) edited by Russell 0. Potts and Richard H. Guy
(1997). Examples of such devices are disclosed in U.S. Pat. Nos.
5,146,846; 5,223,262; 4,820,724; 4,379,454; and 4,956,171; and U.S.
Patent Publication No. US20110300198, all of which are incorporated
herein by reference in their entirety and such descriptions are not
meant to be limiting. The transdermal mode of storing and
delivering the compositions onto the skin, including hair, and
forming the active composition is convenient and well-suited for
the purposes of an embodiment of the present invention. In one
embodiment method, the application occurs through a sustained
release vehicle, carrier, or diluent, e.g., a topically applied
sustained released patch. In one embodiment, when a topical patch
is used, the patch is applied to the desired area for extended
period of time. In one embodiment, the extended period of time is
greater than one hour, most in one embodiment the extended period
of time is overnight, i.e., when the user is sleeping.
Additionally, the transdermal patches may be formulated to provide
extended benefits for a period of about 1-7 days, in one
embodiment, about 2 to 7 days, in one embodiment about 3-7
days.
[0078] The topical compositions can include one or more
cosmetically acceptable vehicles. Such vehicles may take the form
of any known in the art suitable for application to skin and may
include water (e.g., deionized water); vegetable oils; mineral
oils; esters such as octal palmitate, isopropyl myristate and
isopropyl palmitate; ethers such as dicapryl ether and dimethyl
isosorbide; alcohols such as ethanol and isopropanol; fatty
alcohols such as cetyl alcohol, cetearyl alcohol, stearyl alcohol
and biphenyl alcohol; isoparaffins such as isooctane, isododecane
and is hexadecane; silicone oils such as cyclomethicone,
dimethicone, dimethicone cross-polymer, polysiloxanes and their
derivatives, in one embodiment organomodified derivatives;
hydrocarbon oils such as mineral oil, petrolatum, isoeicosane and
polyisobutene; polyols such as propylene glycol, glycerin, butylene
glycol, pentylene glycol and hexylene glycol; waxes such as beeswax
and botanical waxes; or any combinations or mixtures of the
foregoing.
[0079] The vehicle may comprise an aqueous phase, an oil phase, an
alcohol, a silicone phase or mixtures thereof. The cosmetically
acceptable vehicle may also comprise an emulsion. Non-limiting
examples of suitable emulsions include water-in-oil emulsions,
oil-in-water emulsions, silicone-in-water emulsions,
water-in-silicone emulsions, wax-in-water emulsions,
water-oil-water triple emulsions or the like having the appearance
of a cream, gel or microemulsions. The emulsion may include an
emulsifier, such as a nonionic, anionic or amphoteric
surfactant.
[0080] The oil phase of the emulsion in one embodiment has one or
more organic compounds, including emollients; humectants (such as
butylene glycol, propylene glycol, Methyl gluceth-20, and
glycerin); other water-dispersible or water-soluble components
including thickeners such as veegum or hydroxyalkyl cellulose;
gelling agents, such as high MW polyacrylic acid, i.e. CARBOPOL
934; and mixtures thereof. The emulsion may have one or more
emulsifiers capable of emulsifying the various components present
in the composition.
[0081] The compounds suitable for use in the oil phase include
without limitation, vegetable oils; esters such as octyl palmitate,
isopropyl myristate and isopropyl palmitate; ethers such as
dicapryl ether; fatty alcohols such as cetyl alcohol, stearyl
alcohol and behenyl alcohol; isoparaffins such as isooctane,
isododecane and isohexadecane; silicone oils such as dimethicones,
cyclic silicones, and polysiloxanes; hydrocarbon oils such as
mineral oil, petrolatum, isoeicosane and polyisobutene; natural or
synthetic waxes; and the like. Suitable hydrophobic hydrocarbon
oils may be saturated or unsaturated, have an aliphatic character
and be straight or branched chained or contain alicyclic or
aromatic rings. The oil-containing phase may be composed of a
singular oil or mixtures of different oils.
[0082] Hydrocarbon oils include those having 6-20 carbon atoms, in
one embodiment 10-16 carbon atoms. Representative hydrocarbons
include decane, dodecane, tetradecane, tridecane, and C.sub.8-20
isoparaffins. Paraffinic hydrocarbons are available from Exxon
under the ISOPARS trademark, and from the Permethyl Corporation. In
addition, C.sub.8-20 paraffinic hydrocarbons such as C.sub.12
isoparaffin (isododecane) manufactured by the Permethyl Corporation
having the tradename Permethyl 99A.TM. are also contemplated to be
suitable. Various commercially available C.sub.16 isoparaffins,
such as isohexadecane (having the tradename Permethyl.RTM.) are
also suitable. Examples of in one embodiment volatile hydrocarbons
include polydecanes such as isododecane and isodecane, including
for example, Permethyl-99A (Presperse Inc.) and the C.sub.7-C.sub.8
through C.sub.12-C.sub.15 isoparaffins such as the Isopar Series
available from Exxon Chemicals. A representative hydrocarbon
solvent is isododecane.
[0083] The oil phase may comprise one or more waxes, including for
example, rice bran wax, carnauba wax, ouricurry wax, candelilla
wax, montan waxes, sugar cane waxes, ozokerite, polyethylene waxes,
Fischer-Tropsch waxes, beeswax, microcrystalline wax, silicone
waxes, fluorinated waxes, and any combination thereof.
[0084] Non-limiting emulsifiers include emulsifying waxes,
emulsifying polyhydric alcohols, polyether polyols, polyethers,
mono- or di-ester of polyols, ethylene glycol mono-stearates,
glycerin mono-stearates, glycerin di-stearates, silicone-containing
emulsifiers, soya sterols, fatty alcohols such as cetyl alcohol,
acrylates, fatty acids such as stearic acid, fatty acid salts, and
mixtures thereof. In one embodiment, the emulsifiers may include
soya sterol, cetyl alcohol, stearic acid, emulsifying wax,
acrylates, silicone containing emulsifiers and mixtures thereof.
Other specific emulsifiers that can be used in the composition of
the present invention include, but are not limited to, one or more
of the following: C.sub.10-30 alkyl acrylate crosspolymer;
Dimethicone PEG-7 isostearate, acrylamide copolymer; mineral oil;
sorbitan esters; polyglyceryl-3-diisostearate; sorbitan
monostearate, sorbitan tristearate, sorbitan sesquioleate, sorbitan
monooleate; glycerol esters such as glycerol monostearate and
glycerol monooleate; polyoxyethylene phenols such as
polyoxyethylene octyl phenol and polyoxyethylene nonyl phenol;
polyoxyethylene ethers such as polyoxyethylene cetyl ether and
polyoxyethylene stearyl ether; polyoxyethylene glycol esters;
polyoxyethylene sorbitan esters; dimethicone copolyols;
polyglyceryl esters such as polyglyceryl-3-diisostearate; glyceryl
laurate; Steareth-2, Steareth-10, and Steareth-20, to name a few.
Additional emulsifiers are provided in the INCI Ingredient
Dictionary and Handbook 11.sup.th Edition 2006, the disclosure of
which is hereby incorporated by reference.
[0085] These emulsifiers typically will be present in the
composition in an amount from about 0.001% to about 10% by weight,
in particular in an amount from about 0.01% to about 5% by weight,
and more in one embodiment, from about 0.1% to about 3% by
weight.
[0086] The oil phase may comprise one or more volatile and/or
non-volatile silicone oils. Volatile silicones include cyclic and
linear volatile dimethylsiloxane silicones. In one embodiment, the
volatile silicones may include cyclodimethicones, including
tetramer (D.sub.4), pentamer (D.sub.5), and hexamer (D.sub.6)
cyclomethicones, or mixtures thereof. Particular mention may be
made of the volatile cyclomethicone-hexamethyl cyclotrisiloxane,
octamethyl-cyclotetrasiloxane, and decamethyl-cyclopentasiloxane.
Suitable dimethicones are available from Dow Corning under the name
Dow Corning 200.RTM. Fluid and have viscosities ranging from 0.65
to 600,000 centistokes or higher. Suitable non-polar, volatile
liquid silicone oils are disclosed in U.S. Pat. No. 4,781,917,
herein incorporated by reference in its entirety. Additional
volatile silicones materials are described in Todd et al.,
"Volatile Silicone Fluids for Cosmetics", Cosmetics and Toiletries,
91:27-32 (1976), herein incorporated by reference in its entirety.
Linear volatile silicones generally have a viscosity of less than
about 5 centistokes at 25.degree. C., whereas the cyclic silicones
have viscosities of less than about 10 centistokes at 25.degree. C.
Examples of volatile silicones of varying viscosities include Dow
Corning 200, Dow Corning 244, Dow Corning 245, Dow Corning 344, and
Dow Corning 345, (Dow Corning Corp.); SF-1204 and SF-1202 Silicone
Fluids (G.E. Silicones), GE 7207 and 7158 (General Electric Co.);
and SWS-03314 (SWS Silicones Corp.). Linear, volatile silicones
include low molecular weight polydimethylsiloxane compounds such as
hexamethyldisiloxane, octamethyltrisiloxane,
decamethyltetrasiloxane, and dodecamethylpentasiloxane, to name a
few.
[0087] Non-volatile silicone oils will typically comprise
polyalkylsiloxanes, polyarylsiloxanes, polyalkylarylsiloxanes, or
mixtures thereof. Polydimethylsiloxanes are in one embodiment
non-volatile silicone oils. The non-volatile silicone oils will
typically have a viscosity from about 10 to about 60,000
centistokes at 25.degree. C., in one embodiment between about 10
and about 10,000 centistokes, in one embodiment between about 10
and about 500 centistokes; and a boiling point greater than
250.degree. C. at atmospheric pressure. Non limiting examples
include dimethyl polysiloxane (dimethicone), phenyl trimethicone,
and diphenyldimethicone. The volatile and non-volatile silicone
oils may optionally be substituted with various functional groups
such as alkyl, aryl, amine groups, vinyl, hydroxyl, haloalkyl
groups, alkylaryl groups, and acrylate groups, to name a few.
[0088] The water-in-silicone emulsion may be emulsified with a
nonionic surfactant (emulsifier) such as, for example,
polydiorganosiloxane-polyoxyalkylene block copolymers, including
those described in U.S. Pat. No. 4,122,029, the disclosure of which
is hereby incorporated by reference. These emulsifiers generally
comprise a polydiorganosiloxane backbone, typically
polydimethylsiloxane, having side chains comprising-(EO)m- and/or
--(PO)n- groups, where EO is ethyleneoxy and PO is
1,2-propyleneoxy, the side chains being typically capped or
terminated with hydrogen or lower alkyl groups (e.g., C1-6,
typically C1-3). Other suitable water-in-silicone emulsifiers are
disclosed in U.S. Pat. No. 6,685,952, the disclosure of which is
hereby incorporated by reference herein. Commercially available
water-in-silicone emulsifiers include those available from Dow
Corning under the trade designations 3225C and 5225C FORMULATION
AID; SILICONE SF-1528 available from General Electric; ABIL EM 90
and EM 97, available from Goldschmidt Chemical Corporation
(Hopewell, Va.); and the SILWET series of emulsifiers sold by OSI
Specialties (Danbury, Conn.).
[0089] Examples of water-in-silicone emulsifiers include, but are
not limited to, dimethicone PEG 10/15 crosspolymer, dimethicone
copolyol, cetyl dimethicone copolyol, PEG-15 lauryl dimethicone
crosspolymer, laurylmethicone crosspolymer, cyclomethicone and
dimethicone copolyol, dimethicone copolyol (and) caprylic/capric
triglycerides, polyglyceryl-4 isostearate (and) cetyl dimethicone
copolyol (and) hexyl laurate, and dimethicone copolyol (and)
cyclopentasiloxane. In one embodiment examples of water-in-silicone
emulsifiers include, without limitation, PEG/PPG-18/18 dimethicone
(trade name 5225C, Dow Corning), PEG/PPG-19/19 dimethicone (trade
name BY25-337, Dow Corning), Cetyl PEG/PPG-10/1 dimethicone (trade
name Abil EM-90, Goldschmidt Chemical Corporation), PEG-12
dimethicone (trade name SF 1288, General Electric), lauryl
PEG/PPG-18/18 methicone (trade name 5200 FORMULATION AID, Dow
Corning), PEG-12 dimethicone crosspolymer (trade name 9010 and 9011
silicone elastomer blend, Dow Corning), PEG-10 dimethicone
crosspolymer (trade name KSG-20, Shin-Etsu), dimethicone PEG-10/15
crosspolymer (trade name KSG-210, Shin-Etsu), and dimethicone PEG-7
isostearate.
[0090] The water-in-silicone emulsifiers typically will be present
in the composition in an amount from about 0.001% to about 10% by
weight, in particular in an amount from about 0.01% to about 5% by
weight, and more in one embodiment, below 1% by weight.
[0091] The aqueous phase of the emulsion may include one or more
additional solvents, including lower alcohols, such as ethanol,
isopropanol, and the like. The volatile solvent may also be a
cosmetically acceptable ester such as butyl acetate or ethyl
acetate; ketones such as acetone or ethyl methyl ketone; or the
like.
[0092] The oil-containing phase will typically comprise from about
10% to about 99%, in one embodiment from about 20% to about 85%,
and more in one embodiment from about 30% to about 70% by weight,
based on the total weight of the emulsion, and the aqueous phase
will typically comprise from about 1% to about 90%, in one
embodiment from about 5% to about 70%, and more in one embodiment
from about 20% to about 60% by weight of the total emulsion. The
aqueous phase will typically comprise from about 25% to about 100%,
more typically from about 50% to about 95% by weight water.
[0093] The compositions may include liposomes. The liposomes may
comprise other additives or substances and/or may be modified to
more specifically reach or remain at a site following
administration.
[0094] The daily doses recommended in conformity with the invention
range from 0.5 to 2600 mg/day, and in one embodiment from 5 to 1200
mg/day of Hoya carnosa extract. The compositions of the invention
can be taken for several days, weeks or months. The regimen of
treatment can be repeated many times in a year and can even be
continuous.
[0095] The composition may optionally comprise other cosmetic
actives and excipients, obvious to those skilled in the art
including, but not limited to, fillers, emulsifying agents,
antioxidants, surfactants, film formers, chelating agents, gelling
agents, thickeners, emollients, humectants, moisturizers, vitamins,
minerals, viscosity and/or rheology modifiers, sunscreens,
keratolytics, depigmenting agents, retinoids, hormonal compounds,
alpha-hydroxy acids, alpha-keto acids, anti-mycobacterial agents,
antifungal agents, antimicrobials, antivirals, analgesics, lipidic
compounds, anti-allergenic agents, H1 or H2 antihistamines,
anti-inflammatory agents, anti-irritants, antineoplastics, immune
system boosting agents, immune system suppressing agents, anti-acne
agents, anesthetics, antiseptics, insect repellents, skin cooling
compounds, skin protectants, skin penetration enhancers,
exfollients, lubricants, fragrances, colorants, depigmenting
agents, hypopigmenting agents, preservatives (e.g., DMDM
Hydantoin/lodopropynylbutylcarbonate), stabilizers, pharmaceutical
agents, photostabilizing agents, neutralizers (e.g.,
triethanolamine) and mixtures thereof. In addition to the
foregoing, the cosmetic compositions of the invention may contain
any other compound for the treatment of skin disorders.
[0096] The composition may comprise additional active ingredients
having anti-aging benefits, as it is contemplated that synergistic
improvements may be obtained with such combinations. Exemplary
anti-aging components include, without limitation, botanicals
(e.g., Butea Frondosa extract); thiodipropionic acid (TDPA) and
esters thereof; retinoids (e.g., all-trans retinoic acid, 9-cis
retinoic acid, phytanic acid and others); hydroxy acids (including
alpha-hydroxyacids and beta-hydroxyacids), salicylic acid and
salicylates; exfoliating agents (e.g., glycolic acid,
3,6,9-trioxaundecanedioic acid, etc.); estrogen synthetase
stimulating compounds (e.g., caffeine and derivatives); compounds
capable of inhibiting 5 alpha-reductase activity (e.g., linolenic
acid, linoleic acid, finasteride, and mixtures thereof); barrier
function enhancing agents (e.g., ceramides, glycerides, cholesterol
and its esters, alpha-hydroxy and omega-hydroxy fatty acids and
esters thereof, etc.); collagenase inhibitors; and elastase
inhibitors; to name a few.
[0097] The present compositions may also include skin whiteners.
Some examples of such suitable skin whiteners include, but are not
limited to, one or more of the following: ascorbyl glucoside,
vitamin C, retinol and/or its derivatives, arbutin, bearberry
extract, rumex crispus extract, milk proteins including hydrolyzed
milk proteins, N,N,S-tris(carboxym-ethyl)cysteamine, oleanolic
acids, perilla oil, placenta extract, Saxifragia sarmentosa,
perilla extract, juniperic acid, TDPA, Ligusticum chiangxiong
hart., Asmunda japonica thunb., Stellaria medica (L.) cyr., Sedum
sarmentosum bunge, Ligusticum lucidum Ait., ilex purpurea hassk,
emblica, apigenin, ascorbyl palmitol, carruba polyphenols,
hesperitin, inabata polyphenol, isoliquirtigenin,
kaempherol-7-neohesperidose, L-mimosine, luteolin, oil-soluble
licorice extract P-T(40), oxa acid, phenyl isothiocyanate, cococin,
silymarin, T4CA, teterahydro curcumin, unitrienol,
ursolic-oleanolic acid, UVA/URSI, hydroquinone, kojic acid,
Glycyrrhiza glabra, Chiarella vulgaris extract, coconut fruit
extract, Butea frondosa, Naringi crenulata, Stenoloma chusana,
Azadirachta indicia, Morinda citrifolia, or any combinations
thereof, see U.S. Pat. No. 7,189,419 herby incorporated by
reference in its entirety.
[0098] Suitable hydroxyl acids include, for example, glycolic acid,
lactic acid, malic acid, tartaric acid, citric acid,
2-hydroxyalkanoic acid, mandelic acid, salicylic acid, and alkyl
derivatives thereof, including 5-n-octanoylsalicylic acid,
5-n-dodecanoylsalicylic acid, 5-n-decanoylsalicylic acid,
5-n-octylsalicylic acid, 5-n-heptyloxysalicylic acid,
4-n-heptyloxysalicylic acid, and 2-hydroxy-3-methylbenzoic acid or
alkoxy derivatives thereof, such as 2-hydroxy-3-methyoxybenzoic
acid.
[0099] Exemplary retinoids include, without limitation, retinoic
acid (e.g., all-trans or 13-cis) and derivatives thereof, retinol
(Vitamin A) and esters thereof, such as retinol palmitate, retinol
acetate and retinol propionate, and salts thereof.
[0100] In another embodiment, the topical compositions of the
present invention may also include one or more of the following: a
skin penetration enhancer, an emollient, a skin plumper, an optical
diffuser, a sunscreen, an exfoliating agent, and an
antioxidant.
[0101] An emollient provides the functional benefits of enhancing
skin texture (smoothness) and reducing the appearance of fine lines
and coarse wrinkles. Examples include isopropyl myristate,
petrolatum, isopropyl lanolate, silicones (e.g., methicone,
dimethicone), oils, mineral oils, fatty acid esters, cetyl
ethylhexanoate, C.sub.12-15 alkyl benzoate, isopropyl isostearate,
diisopropyl dimer dillinoeate, or any mixtures thereof. The
emollient may be in one embodiment present from about 0.1 wt % to
about 50 wt % of the total weight of the composition.
[0102] A skin plumper serves as a collagen enhancer to the skin. An
example of a suitable and in one embodiment skin plumper is
palmitoyl oligopeptide. Other skin plumpers are collagen and/or
other glycosaminoglycan (GAG) enhancing agents. When present, the
skin plumper may comprise from about 0.1 wt % to about 20 wt % of
the total weight of the composition.
[0103] An optical diffuser is a particle that changes the surface
optometrics of skin, resulting in a visual blurring and softening
of, for example, lines and wrinkles. Examples of optical diffusers
that can be used in the present invention include, but are not
limited to, boron nitride, mica, nylon, polymethylmethacrylate
(PMMA), polyurethane powder, sericite, silica, silicone powder,
talc, Teflon, titanium dioxide, zinc oxide, or any mixtures
thereof. When present, the optical diffuser may be present from
about 0.01 wt % to about 20 wt % of the total weight of the
composition.
[0104] A sunscreen for protecting the skin from damaging
ultraviolet rays may also be included. In one embodiment sunscreens
are those with a broad range of UVB and UVA protection, such as
octocrylene, avobenzone (Parsol 1789), octyl methoxycinnamate,
octyl salicylate, oxybenzone, homosylate, benzophenone, camphor
derivatives, zinc oxide, and titanium dioxide. When present, the
sunscreen may comprise from about 0.01 wt % to about 70 wt % of the
composition.
[0105] Suitable exfoliating agents include, for example,
alpha-hydroxyacids, beta-hydroxyacids, oxaacids, oxadiacids, and
their derivatives such as esters, anhydrides and salts thereof.
Suitable hydroxy acids include, for example, glycolic acid, lactic
acid, malic acid, tartaric acid, citric acid, 2-hydroxyalkanoic
acid, mandelic acid, salicylic acid and derivatives thereof. A in
one embodiment exfoliating agent is glycolic acid. When present,
the exfoliating agent may comprise from about 0.1 wt % to about 80
wt % of the composition.
[0106] An antioxidant functions, among other things, to scavenge
free radicals from skin to protect the skin from environmental
aggressors. Examples of antioxidants that may be used in the
present compositions include compounds having phenolic hydroxy
functions, such as ascorbic acid and its derivatives/esters;
alpha-hydroxyacids; beta-carotene; catechins; curcumin; ferulic
acid derivatives (e.g. ethyl ferulate, sodium ferulate); gallic
acid derivatives (e.g., propyl gallate); lycopene; reductic acid;
rosmarinic acid; tannic acid; tetrahydrocurcumin; tocopherol and
its derivatives (e.g., tocopheryl acetate); uric acid; or any
mixtures thereof. Other suitable antioxidants are those that have
one or more thiol functions (--SH), in either reduced or
non-reduced form, such as glutathione, lipoic acid, thioglycolic
acid, and other sulfhydryl compounds. The antioxidant may be
inorganic, such as bisulfites, metabisulfites, sulfites, or other
inorganic salts and acids containing sulfur. Compositions of the
present invention may comprise an antioxidant in one embodiment
from about 0.001 wt % to about 10 wt %, and more in one embodiment
from about 0.01 wt % to about 5 wt %, of the total weight of the
composition.
[0107] In some embodiments, additional actives may include a
collagen stimulator and/or an elastin stimulator, e.g., a substance
that stimulates elastin production, and/or a glycosaminoglycan
enhancer. Examples of collagen, elastin, and glycosaminoglycan
enhancers include, e.g., fennel extract, carrot extract, and
alfalfa extract. In some embodiments the additional actives may
include a collagenase inhibitor and/or elastase inhibitor.
[0108] In some embodiments the cosmetic compositions can further
comprise at least one collagen and/or elastin stimulator. Such
collagen or elastin stimulators are effective in, for example,
providing improvement in procollagen and/or collagen production
and/or improvement in maintenance and remodeling of elastin.
[0109] Colorants may include, for example, organic and inorganic
pigments and pearlescent agents. Suitable inorganic pigments
include, but are not limited to, titanium oxide, zirconium oxide,
and cerium oxide, as well as zinc oxide, iron oxide, chromium oxide
and ferric blue. Suitable organic pigments include barium,
strontium, calcium, aluminium lakes and carbon black. Suitable
pearlescent agents include mica coated with titanium oxide, iron
oxide, or natural pigments.
[0110] Various fillers and additional components may be added.
Fillers are normally present in an amount of about 0 weight % to
about 20 weight %, based on the total weight of the composition, in
one embodiment about 0.1 weight % to about 10 weight %. Suitable
fillers include without limitation the following: silica, treated
silica, talc, zinc stearate, mica, kaolin, Nylon powders such as
Orgasol.TM., polyethylene powder, Teflon.TM., starch, boron
nitride, copolymer microspheres such as Expancel.TM. (Nobel
Industries), Polytrap.TM. (Dow Corning) and silicone resin
microbeads (Tospearl.TM. from Toshiba), and the like.
[0111] In one embodiment of the invention, the compositions may
include additional skin actives such as, but not limited to,
botanicals, keratolytic agents, desquamating agents, keratinocyte
proliferation enhancers, collagenase inhibitors, elastase
inhibitors, depigmenting agents, anti-inflammatory agents,
steroids, anti-acne agents, antioxidants, salicylic acid or
salicylates, anti-lipid agents, thiodipropionic acid or esters
thereof, and advanced glycation end-product (AGE) inhibitors.
[0112] In a specific embodiment, the composition may comprise at
least one additional botanical, such as, for example, a botanical
extract, an essential oil, or the plant itself. Suitable botanicals
include, without limitation, extracts from Abies pindrow, Acacia
catechu, Anogeissus latifolia, Asmunda japonica, Azadirachta
indica, Butea frondosa, Butea monosperma, Cedrus deodara, Emblica
officinalis, Ficus benghalensis, Glycyrrhiza glabra, Ilex purpurea
Hassk, Inula racemosa, Ligusticum chuangxiong, Ligusticum lucidum,
Mallotus philippinensis, Mimusops elengi, Morinda citrifolia,
Moringa oleifera, Naringi crenulata, Nerium indicum, Psoralea
corylifolia, Stenoloma chusana, Terminalia bellerica, tomato
glycolipid and mixtures thereof.
[0113] Other conventional additives include: vitamins, such as
tocopherol and ascorbic acid; vitamin derivatives such as ascorbyl
monopalmitate; thickeners such as hydroxyalkyl cellulose; gelling
agents; structuring agents such as bentonite, smectite, magnesium
aluminum silicate and lithium magnesium silicate; metal chelating
agents such as EDTA; pigments such as zinc oxide and titanium
dioxide; colorants; emollients; and humectants.
[0114] In one embodiment, the composition is essentially free of
components having a strong oxidizing potential, including for
example, organic or inorganic peroxides. "Essentially free of"
these components means that the amounts present are insufficient to
have a measurable impact on the activity of an extract of Hoya
carnosa. In some embodiments, this will be, in relation to the
amount of Hoya carnosa, less than 1% by weight.
[0115] In one embodiment, the composition of the invention
comprising an extract of Hoya carnosa may have a pH between about 1
and about 8. In certain embodiments, the pH of the composition will
be acidic, i.e., less than 7.0, and in one embodiment will be
between about 2 and about 7, more in one embodiment between about
3.5 and about 5.5.
[0116] Method of Treating Aging or Aged skin
[0117] The invention provides a method for treating aging skin by
topically applying a composition comprising an extract of Hoya
carnosa, in one embodiment in a cosmetically acceptable vehicle,
over the affected area for a period of time sufficient to reduce,
ameliorate, reverse or prevent dermatological signs of aging. This
method is particularly useful for treating signs of skin photoaging
and intrinsic aging.
[0118] Generally, the improvement in the condition and/or aesthetic
appearance is selected from the group consisting of: reducing
dermatological signs of chronological aging, photo-aging, hormonal
aging, and/or actinic aging; preventing and/or reducing the
appearance of lines and/or wrinkles; reducing the noticeability of
facial lines and wrinkles, facial wrinkles on the cheeks, forehead,
perpendicular wrinkles between the eyes, horizontal wrinkles above
the eyes, and around the mouth, marionette lines, and particularly
deep wrinkles or creases; preventing, reducing, and/or diminishing
the appearance and/or depth of lines and/or wrinkles; improving
lipid accumulation in adipocytes; improving the appearance of
suborbital lines and/or periorbital lines; reducing the appearance
of crow's feet; rejuvenating and/or revitalizing skin, particularly
aging skin; reducing skin fragility; preventing and/or reversing of
loss of glycosaminoglycans and/or collagen; ameliorating the
effects of estrogen imbalance; preventing skin atrophy; preventing,
reducing, and/or treating hyperpigmentation; minimizing skin
discoloration; improving skin tone, radiance, clarity and/or
tautness; preventing, reducing, and/or ameliorating skin sagging;
improving skin firmness, plumpness, suppleness and/or softness;
improving procollagen and/or collagen production; improving skin
texture and/or promoting retexturization; improving skin barrier
repair and/or function; improving the appearance of skin contours;
restoring skin luster and/or brightness; minimizing dermatological
signs of fatigue and/or stress; resisting environmental stress;
replenishing ingredients in the skin decreased by aging and/or
menopause; improving communication among skin cells; increasing
cell proliferation and/or multiplication; increasing skin cell
metabolism decreased by aging and/or menopause; retarding cellular
aging; improving skin moisturization; enhancing skin thickness;
increasing skin elasticity and/or resiliency; enhancing
exfoliation; improving microcirculation; and any combinations
thereof.
[0119] The composition will typically be applied to the skin one,
two, or three times daily for as long as is necessary to achieve
desired anti-aging results. The treatment regimen may comprise
daily application for at least one week, at least two weeks, at
least four weeks, at least eight weeks, or at least twelve weeks.
Chronic treatment regimens are also contemplated.
[0120] A composition comprising an extract of Hoya carnosa is
topically applied to an "individual in need thereof," by which is
meant an individual that stands to benefit from reducing visible
signs of skin damage or aging. In a specific embodiment, the Hoya
carnosa extract is provided in a pharmaceutically, physiologically,
cosmetically, and dermatologically-acceptable vehicle, diluent, or
carrier, where the composition is topically applied to an affected
area of skin and left to remain on the affected area in an amount
effective for improving the condition and aesthetic appearance of
skin.
[0121] In one embodiment, methods for treating fine lines and
wrinkles comprise topically applying the inventive compositions
comprising a Hoya carnosa extract to the skin of an individual in
need thereof, e.g., topically application directly to the fine line
and/or wrinkle in an amount and for a time sufficient to reduce the
severity of the fine lines and/or wrinkles or to prevent or inhibit
the formation of new fine lines and/or wrinkles. The effect of a
composition on the formation or appearance of fine lines and
wrinkles can be evaluated qualitatively, e.g., by visual
inspection, or quantitatively, e.g., by microscopic or computer
assisted measurements of wrinkle morphology (e.g., the number,
depth, length, area, volume and/or width of wrinkles per unit area
of skin). This embodiment includes treatment of wrinkles on the
skin of the hands, arms, legs, neck, chest, and face, including the
forehead.
[0122] It is also contemplated that the compositions of the
invention will be useful for treating thin skin by topically
applying the composition to thin skin of an individual in need
thereof. In some embodiments, the treatment is for thin skin in
men, whereas other embodiments treat thin skin in women,
pre-menopausal or post-menopausal, as it is believed that skin
thins differently with age in men and women, and in particular in
women at different stages of life.
[0123] The method of the invention may be employed prophylactically
to forestall aging including in patients that have not manifested
signs of skin aging, most commonly in individuals under 25 years of
age. The method may also reverse or treat signs of aging once
manifested as is common in patients over 25 years of age.
EXAMPLES
[0124] The following examples describe specific aspects of the
invention to illustrate the invention but should not be construed
as limiting the invention, as the examples merely provide specific
methodology useful in the understanding and practice of the
invention and its various aspects.
Example 1
Preparation of Hoya carnosa Extract
[0125] I. Extraction Protocol 1
[0126] 250 g of dried and powdered material derived from the whole
of the Hoya carnosa was percolated with 1000 ml EtOH/H.sub.2O
(50:50, v/v) at room temperature for 24 hours. This percolation was
repeated 2 times and then the EtOH/H.sub.2O extraction solution was
concentrated under vacuum by rotary evaporator at 40-50.degree. C.
to 150 ml or end of distillation, whichever occurs first.
[0127] The concentrated solution was then diluted with pure water
to 1500 ml of volume and sonicated for 20 minutes to generate an
aqueous suspension. The suspension was left to stand at 4.degree.
C. for 12 h and then centrifuged. The supernatant was then
transferred to a separation funnel where three separate extraction
were done with 500 ml of hexane each. The hexane solvent was
recycled, and the hexane extract was discarded.
[0128] Charcoal (10% by w. vs. total dry matter content) was then
added to the aqueous phase yielded from the hexane extraction and
stirred for 1 hour. The solution was then filtered and concentrated
under vacuum at 40-50.degree. C. to adjust the concentration of
solution to 5% (w/v) of its dry matter. The adjusted solution was
then passed through a Diaion HP-20 column (20 times of the dry
weight,) and washed successively with:
[0129] 1) H20: 2 times Diaion HP-20 column volume (100 g HP-20 is
equal to 210 ml of column volume);
[0130] 2) 20% aqueous EtOH: 2 times Diaion HP-20 column volume;
[0131] 3) 50% aqueous EtOH: 2 times Diaion HP-20 column volume;
[0132] 4) 95% aqueous EtOH: 3 times Diaion HP-20 column volume.
[0133] The elutents of washes 1-4 were concentrated, respectively,
to dryness to obtain fractions 1-4.
[0134] Extraction Protocol 2 (Exemplary)
[0135] An amount (g) of chopped Hoya carnosa flowers may be
gathered and pulverized. Subsequently, reflux extraction, using
methods known to those of ordinary skill in the art, may be
conducted using 8-10.times. the weight of the pulverized flowers of
water at 100.degree. C. This step may be repeated. The resulting
extract may be filtered and condensed using methods known to those
of ordinary skill in the art, after which the extract may undergo
vacuum distillation at appropriate conditions known to those of
ordinary skill in the art. Subsequently, the extract may be mixed
with a suitable amount of dextrin and spray dried.
[0136] As noted in the remaining specification, modifications and
adaptations of the above-noted extraction process are possible,
particularly during a scale-up to larger volumes for
production.
[0137] II. HPLC
[0138] The extract was then characterized by high performance
liquid chromatography. A sample size of approximately 5 mg/mL was
dispersed in 25/75 MeOH/H.sub.2O and sonicated. The
characterization was performed on a Zorbax SBC-18 column (7.5
cm.times.4.6 mm, 3.5 um particle size) and detection was achieved
using diode array UV absorbance, 260 nm 300 nm and 360 nm, with
lines on FIG. 1 depicted in ascending order and 260 nm on bottom.
Operating conditions were flow rate 1.5 ml/min; temperature,
40.degree. C.; sample injection volume, 20 .mu.L, and time of run,
19 minutes. The mobile phase gradient used was as follows. In one
embodiment, the extracted composition of the present invention, in
substantial isolation, exhibits an HPLC profile substantially
similar to that depicted in FIG. 1.
TABLE-US-00001 TABLE 1 Mobile Phase Gradient Time Phase 0 Minutes:
15% Methanol(Solvent B)/85% Water with 1% acetic acid (Solvent A)
10 Minutes: 95% Methanol/5% Water with 1% Acetic acid. 15 Minutes:
15% Methanol/85% Water with1% Acetic acid. 15.01 Minutes 95%
Methanol/5% Water with1% Acetic acid. 19 Minutes: 15% Methanol/85%
Water with1% Acetic acid
[0139] The HPLC characterization of the extract is displayed in
FIG. 1.
Example 2
In Vivo Up-Regulation of Key Skin Biomarkers
[0140] Botanical extracts of Hoya carnosa were tested for the
ability to upregulate skin biomarkers in vivo. 20 healthy female
Caucasian subjects aged 30-65 with skin type II or III and mild to
moderate photo damage were treated with ingredients on the dorsal
forearm for 3 weeks (3 consecutive rounds of 5.times.24 hour
patches under semi-occlusion). Test articles and vehicles were
applied in a randomized allocation on five sites on each forearm.
Each subject was treated with the extract of Hoya carnosa at a
concentration of 0.2% formulated in Propylene
Glycol/Ethanol/H.sub.2O (65:25:10) vehicle and the vehicle control.
The application dose was 2 mg/cm.sup.2. After treatment, a 2 mm
punch biopsy was obtained from each treatment site and fixed in 10%
buffered formalin. Tissue samples were then embedded in paraffin,
sectioned (5 micrometer thickness), processed and stained for the
following skin markers--Total Collagen (by Masson Trichrome) and
Pro-collagen. In addition, epidermal thickness was evaluated. For
each marker, the treated site was compared to the vehicle site to
determine the difference in the intensity of the marker. If the
intensity of the marker in the treated site is higher relative to
control, it indicates improvement of that biomarker. Table 2 shows
the percent of subjects that had an improvement in the tested skin
biomarkers after three weeks of treatment with an extract of Hoya
carnosa.
TABLE-US-00002 TABLE 2 Percent of subjects that had an improvement
in the tested skin biomarkers after three weeks of treatment with
an extract of Hoya carnosa. Active Test rate Epidermal Total pro-
ingredients (% active) Thickening Collagen Collagen Hoya carnosa
0.200 35.3 45.7 33.3 (Thumb.)
[0141] The botanical extract of Hoya carnosa upregulated biomarkers
such as epidermal thickening (35.3% of subjects exhibited an
increase), collagen (45.7% of subjects exhibited an increase), and
pro-collagen (33.3% of subjects exhibited an increase), in vivo
when topically applied to skin. It is believed that the
up-regulation of these biomarkers, which decline in aging skin,
leads to an improvement in the appearance of aging or aged
skin.
Example 3
Modulation of Intracellular Triglycerides
[0142] Cryopreserved human primary pre-adipocytes harvested from
the subcutaneous adipose tissue of a healthy female were obtained
from Zen-Bio (Research Triangle Park, N.C.). Following the
manufacturer's instructions, the pre-adipocytes were cultured in
Preadipocyte Medium containing DMEM/Ham's F-12 (1:1, v/v). After
reaching 90% confluence, the pre-adipocytes were induced to
differentiate into adipocytes by changing into Adipocyte
Differentiation Medium in presence or absence of test actives.
Treatment with test actives was repeated 3 days after initiation of
differentiation. After 7 days from initiation of differentiation,
medium was replaced with Maintenance Medium, in presence or absence
of test actives and the adipocytes are incubated for another 3
days. The production of triglycerides in the adipocytes was
determined by using a triglyceride assay kit (Zen-Bio). Results
were obtained in triplicate and statistical significance of results
was determined using a t-test.
[0143] Use of a extract of Hoya carnosa at a medium concentration
of 0.10% yielded at least a 20% increase in intracellular
triglycerides relative to the control. It is therefore expected
that use of a extract of Hoya carnosa at varying concentration will
yield increased concentration of intracellular trigylcerides in the
treated cells.
Exemplary Compositions
[0144] Cosmetic compositions comprising an extract of Hoya carnosa
for topical application to skin are provided in Tables 3-4
below.
TABLE-US-00003 TABLE 3 Sample Anti-Aging Facial Cosmetic
Composition Ingredient Aesthetic modifier Emollient Emulsifier
Anti-inflammation agent Chelater Coolant Elastin stimulator
Exfoliator Fragrance Humectant Microcirculation enhancer
Neutralizer Preservative Sunscreen Collagenase/elastinase inhibitor
Phytol Antioxidant Fennel Extract Carrot extract Pomegranate
extract Thiodipropionic acid (TDPA) Green tea polyphenol L-4
Thiazolylanine Hoya carnosa extract Demineralized water
TABLE-US-00004 TABLE 4 Sample Skin Lightening Compositions
Description Demineralized Water Carbopol 934 Acrylates/C10-30 Alkyl
Acrylate Crosspolymer Acrylates/C10-30 Alkyl Acrylate Crosspolymer
Xanthan Gum Disodium EDTA - Tech Grade Methylparaben Alcohol SD40B
Alcohol Mixture (3210&1901 92.52-7.48) Alcohol Mixture
(3215&1901 92.52-7.48) Phenoxyethanol-98% MIN (*RI*) Butylene
Glycol Pentylene Glycol (*RI*) Ethoxydiglycol ISODODECANE Dilauryl
Thiodipropionate Tetrahexyldecyl Ascorbate Ascorbyl Glucoside
Glycyrrhizinate - Dipotassium Unp. Silica Shells Sodium Hydroxide
Solution 50% Silicone Fluid SF-96-5 PEG-40 Stearate Steareth-2
Saxifraga Sarmentosa/Grape Extract Saccharomyces/Zinc ferment Yeast
Extract Kudzu (Pueraria Lobate) Symbiosome extract Soybean (Gly.
Soja) Extract Carrot (Daucus Carota Sativa) Root Extract Phytol
Dimethicone/Dimethicone Crosspolymer Thiodipropionic Acid H.
carnosa Extract
[0145] These anti-aging compositions are believed to be effective
to treat, reverse, ameliorate and/or prevent signs of aging,
specifically, the compositions are believed to reduce the
appearance of wrinkles, lines, and sagging in the skin. The
compositions of Tables 3-4 are applied to skin in need of
treatment, by which is meant skin in need of an anti-aging benefit.
The cosmetic compositions may be applied directly to the skin in
need of treatment.
[0146] These cosmetic compositions are applied to skin aged skin,
folds, sunken appearance and/or hyperpigmented skin, two or three
times daily for as long as is necessary to achieve desired
anti-aging and/or skin lightening results, a treatment regimen
which may comprise daily application for at least one week, at
least two weeks, at least four weeks, at least eight weeks, or at
least twelve weeks. Alternatively, the exemplary cosmetic
compositions may be used in chronic treatment of aged or discolored
skin.
[0147] All references including patent applications and
publications cited herein are incorporated herein by reference in
their entirety and for all purposes to the same extent as if each
individual publication or patent or patent application was
specifically and individually indicated to be incorporated by
reference in its entirety for all purposes. Many modifications and
variations of this invention can be made without departing from its
spirit and scope, as will be apparent to those skilled in the art.
The specific embodiments described herein are offered by way of
example only, and the invention is to be limited only by the terms
of the appended claims, along with the full scope of equivalents to
which such claims are entitled.
* * * * *